WO2001049871A3 - Process for finding a protease inhibitor - Google Patents

Process for finding a protease inhibitor Download PDF

Info

Publication number
WO2001049871A3
WO2001049871A3 PCT/EP2001/000050 EP0100050W WO0149871A3 WO 2001049871 A3 WO2001049871 A3 WO 2001049871A3 EP 0100050 W EP0100050 W EP 0100050W WO 0149871 A3 WO0149871 A3 WO 0149871A3
Authority
WO
WIPO (PCT)
Prior art keywords
substances
finding
specifically
presenilinase
secretase
Prior art date
Application number
PCT/EP2001/000050
Other languages
French (fr)
Other versions
WO2001049871A2 (en
Inventor
Katja Fechteler
Marcus Kostka
Klaus Fuchs
Christian Haass
Harald Steiner
Original Assignee
Boehringer Ingelheim Pharma
Katja Fechteler
Marcus Kostka
Klaus Fuchs
Christian Haass
Harald Steiner
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Boehringer Ingelheim Pharma, Katja Fechteler, Marcus Kostka, Klaus Fuchs, Christian Haass, Harald Steiner filed Critical Boehringer Ingelheim Pharma
Publication of WO2001049871A2 publication Critical patent/WO2001049871A2/en
Publication of WO2001049871A3 publication Critical patent/WO2001049871A3/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12Q—MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS; COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
    • C12Q1/00—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions
    • C12Q1/34—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving hydrolase
    • C12Q1/37—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving hydrolase involving peptidase or proteinase
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2333/00—Assays involving biological materials from specific organisms or of a specific nature
    • G01N2333/435—Assays involving biological materials from specific organisms or of a specific nature from animals; from humans
    • G01N2333/46—Assays involving biological materials from specific organisms or of a specific nature from animals; from humans from vertebrates
    • G01N2333/47—Assays involving proteins of known structure or function as defined in the subgroups
    • G01N2333/4701—Details
    • G01N2333/4709—Amyloid plaque core protein
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2500/00—Screening for compounds of potential therapeutic value
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2800/00—Detection or diagnosis of diseases
    • G01N2800/28—Neurological disorders
    • G01N2800/2814—Dementia; Cognitive disorders
    • G01N2800/2821—Alzheimer

Abstract

The present invention relates to a process for binding substances capable of specifically inhibiting membrane-bound proteases and a high throughput screening test for finding substances capable of specifically inhibiting η-secretase or presenilinase. The invention further relates to the use of this process or this high throughput screening test for finding substances which are specifically capable of inhibiting η-secretase or presenilinase. It also discloses substances which can be found with a process according to the invention, the use of said substances according to the invention for preparing a medicament for treating neurodegenerative disorders, particularly Alzheimer's disease and pharmaceutical formulations containing the substances according to the invention.
PCT/EP2001/000050 2000-01-06 2001-01-04 Process for finding a protease inhibitor WO2001049871A2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE10000161A DE10000161A1 (en) 2000-01-06 2000-01-06 Determining test substances that inhibit protease, involves incubating cells expressing fusion protein having substrate with cleavage site for protease and reporter, measuring cleaved reporter and comparing with standard
DE10000161.0 2000-01-06

Publications (2)

Publication Number Publication Date
WO2001049871A2 WO2001049871A2 (en) 2001-07-12
WO2001049871A3 true WO2001049871A3 (en) 2002-03-28

Family

ID=7626760

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP2001/000050 WO2001049871A2 (en) 2000-01-06 2001-01-04 Process for finding a protease inhibitor

Country Status (2)

Country Link
DE (1) DE10000161A1 (en)
WO (1) WO2001049871A2 (en)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6579689B2 (en) 2000-05-11 2003-06-17 Scios Inc. Modulation of γ-secretase activity
ES2291917T3 (en) * 2003-09-05 2008-03-01 Cellzome Ag TREATMENT OF NEURODEGENERATIVE DISEASES.
WO2009097416A1 (en) * 2008-01-29 2009-08-06 Vanda Pharmaceuticals, Inc. Imidazolylalkyl- pyridines as dbh inhibitors

Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0534904A1 (en) * 1991-09-23 1993-03-31 Sandoz Ltd. Imidazolylmethyl-pyridines
EP0580161A1 (en) * 1992-07-22 1994-01-26 THE McLEAN HOSPITAL CORPORATION Prophylactic and therapeutic treatment of Alzheimer's disease
EP0778266A1 (en) * 1995-12-05 1997-06-11 Bristol-Myers Squibb Company 5-Amino-6-cyclohexyl-4-hydroxy-hexanamide derivatives as inhibitors of beta-amyloid protein production
WO1998015828A1 (en) * 1996-10-07 1998-04-16 Scios Inc. Method to identify direct inhibitors of the beta-amyloid forming enzyme gamma-secretase
WO1999011801A2 (en) * 1997-09-03 1999-03-11 Zeneca Limited Protease based gene switching system
WO2000003248A1 (en) * 1998-07-09 2000-01-20 Boehringer Ingelheim Pharma Kg Method for identifying a presenilinase inhibitor
WO2001016355A2 (en) * 1999-08-28 2001-03-08 Boehringer Ingelheim Pharma Kg In vitro test system for gamma-secretase from enriched membranes

Patent Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0534904A1 (en) * 1991-09-23 1993-03-31 Sandoz Ltd. Imidazolylmethyl-pyridines
EP0580161A1 (en) * 1992-07-22 1994-01-26 THE McLEAN HOSPITAL CORPORATION Prophylactic and therapeutic treatment of Alzheimer's disease
EP0778266A1 (en) * 1995-12-05 1997-06-11 Bristol-Myers Squibb Company 5-Amino-6-cyclohexyl-4-hydroxy-hexanamide derivatives as inhibitors of beta-amyloid protein production
WO1998015828A1 (en) * 1996-10-07 1998-04-16 Scios Inc. Method to identify direct inhibitors of the beta-amyloid forming enzyme gamma-secretase
WO1999011801A2 (en) * 1997-09-03 1999-03-11 Zeneca Limited Protease based gene switching system
WO2000003248A1 (en) * 1998-07-09 2000-01-20 Boehringer Ingelheim Pharma Kg Method for identifying a presenilinase inhibitor
WO2001016355A2 (en) * 1999-08-28 2001-03-08 Boehringer Ingelheim Pharma Kg In vitro test system for gamma-secretase from enriched membranes

Non-Patent Citations (4)

* Cited by examiner, † Cited by third party
Title
FEEHAN CAROL ET AL: "Shedding of the lymphocyte L-selectin adhesion molecule is inhibited by a hydroxamic acid based protease inhibitor: Identification with an L-selectin-alkaline phosphatase reporter.", JOURNAL OF BIOLOGICAL CHEMISTRY, vol. 271, no. 12, 1996, pages 7019 - 7024, XP000616670, ISSN: 0021-9258 *
HIGAKI JEFFREY N ET AL: "A combinatorial approach to the identification of dipeptide aldehyde inhibitors of beta-amyloid production.", JOURNAL OF MEDICINAL CHEMISTRY, vol. 42, no. 19, pages 3889 - 3898, XP002185434, ISSN: 0022-2623 *
HIROWATARI YUJI ET AL: "A novel method for analysis of viral proteinase activity encoded by hepatitis C virus in cultured cells.", ANALYTICAL BIOCHEMISTRY, vol. 225, no. 1, 1995, pages 113 - 120, XP002096985, ISSN: 0003-2697 *
WOLFE M S ET AL: "TWO TRANSMEMBRANE ASPARTATES IN PRESENILIN-1 REQUIRED FOR PRESENILIN ENDOPROTEOLYSIS AND GAMMA-SECRETASE ACTIVITY", NATURE, MACMILLAN JOURNALS LTD. LONDON, GB, vol. 398, no. 6727, 8 April 1999 (1999-04-08), pages 513 - 517, XP001010554, ISSN: 0028-0836 *

Also Published As

Publication number Publication date
WO2001049871A2 (en) 2001-07-12
DE10000161A1 (en) 2001-07-19

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